Department of BioMolecular Sciences, Division of Medicinal Chemistry, School of Pharmacy, The University of Mississippi, University, MS, United States.
Department of Drug Discovery and Biomedical Sciences, College of Pharmacy and Public Health Sciences, Medical University of South Carolina, Charleston, SC, United States.
Biochim Biophys Acta Gen Subj. 2018 Jan;1862(1):81-196. doi: 10.1016/j.bbagen.2017.08.014. Epub 2017 Aug 24.
The oceans are a uniquely rich source of bioactive metabolites, of which sponges have been shown to be among the most prolific producers of diverse bioactive secondary metabolites with valuable therapeutic potential. Much attention has been focused on marine bioactive peptides due to their novel chemistry and diverse biological properties. As summarized in this review, marine peptides are known to exhibit various biological activities such as antiviral, anti-proliferative, antioxidant, anti-coagulant, anti-hypertensive, anti-cancer, antidiabetic, antiobesity, and calcium-binding activities. This review focuses on the chemistry and biology of peptides isolated from sponges, bacteria, cyanobacteria, fungi, ascidians, and other marine sources. The role of marine invertebrate microbiomes in natural products biosynthesis is discussed in this review along with the biosynthesis of modified peptides from different marine sources. The status of peptides in various phases of clinical trials is presented, as well as the development of modified peptides including optimization of PK and bioavailability.
海洋是具有生物活性代谢物的独特丰富来源，其中海绵已被证明是具有有价值治疗潜力的各种生物活性次生代谢产物的最丰富生产者之一。由于其新颖的化学性质和多样的生物学特性，人们对海洋生物活性肽给予了极大关注。正如本综述所述，海洋肽已知具有多种生物学活性，如抗病毒、抗增殖、抗氧化、抗凝血、抗高血压、抗癌、抗糖尿病、抗肥胖和钙结合活性。本综述重点介绍了从海绵、细菌、蓝细菌、真菌、海鞘和其他海洋来源中分离出的肽的化学和生物学。本文还讨论了海洋无脊椎动物微生物组在天然产物生物合成中的作用，以及不同海洋来源的修饰肽的生物合成。本文还介绍了肽在各个临床试验阶段的状况，以及修饰肽的开发，包括 PK 和生物利用度的优化。
